Nurr1 agonist 29

Chemical Structure : Nurr1 agonist 29

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货号: PC-20768Not For Human Use, Lab Use Only.

Nurr1 agonist 29 is a potent, selective nuclear receptor related 1 (Nurr1, NR4A2) agonist with EC50 of 0.11 uM.

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生物&药学活性

Nurr1 agonist 29 is a potent, selective nuclear receptor related 1 (Nurr1, NR4A2) agonist with EC50 of 0.11 uM.
Nurr1 agonist 29 displays selectivity over DHODH as well as the Nurr1 related receptors Nur77 and NOR1.
Nurr1 agonist 29 exhibits high-affinity binding to the Nurr1 LBD in ITC (Kd = 0.3 μM) and activates full-length human Nurr1 on the monomer (NBRE, EC50=0.22 μM) and the RXR-heterodimer (DR5, EC50=0.36 μM) response elements.
Nurr1 agonist 29 induces mRNA expression of the Nurr1-regulated genes tyrosine hydroxylase (TH) and vesicular amino acid transporter 2 (VMAT2) in Nurr1-expressing human astrocytes (T98G), demonstrating cellular target engagement.
Nurr1 agonist 29 shows no cytotoxic effects in a multiplex toxicity assay in COS-7 cells.
Nurr1 agonist 29 (5 mg/kg) produced a very favorable pharmacokinetic profile in rats with a 4.4 h half-life, 56 μM peak plasma concentration, and 89% bioavailability.

物理化学性质&存储条件

分子量	379.39
分子式	C22H18FNO4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-((3-fluoro-3'-(prop-2-yn-1-yloxy)-[1,1'-biphenyl]-4-yl)carbamoyl)cyclopent-1-ene-1-carboxylic acid

参考文献

1. Jan Vietor, et al. J Med Chem. 2023 May 11;66(9):6391-6402.

Nurr1 agonist 29

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Nurr1 agonist 29

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